These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Optimizing a wet granulation process to obtain high-dose sustained-release tablets with Compritol 888 ATO.
    Author: Rosiaux Y, Girard JM, Desvignes F, Miolane C, Marchaud D.
    Journal: Drug Dev Ind Pharm; 2015; 41(10):1738-44. PubMed ID: 25652358.
    Abstract:
    CONTEXT: Niacin (vitamin B3) is a micronized active pharmaceutical ingredient (API) with poor flow properties making the production of high-dose sustained-release tablets by direct compression a challenge. OBJECTIVE: We evaluated various wet granulation processes as a simple and efficient approach to obtain high-dose (500 and 1000 mg) niacin sustained-release lipid matrix tablets. MATERIALS AND METHODS: A high melting-point lipid (Compritol® 888 ATO) was used as the sustained-release agent. Tablets were prepared by various wet granulation techniques, with different process parameters and binder concentrations to identify the optimal process conditions. RESULTS: A binder (PVP) was needed to increase particle bonding and tablet strength. Process parameters, such as spray rate and quantity of liquid, had only a slight impact on the properties of the granules and resultant tablets, in the presence of low binder concentrations. Increasing binder concentration improved granule wetting, resulting in significant granule growth and improved flow properties. Sustained-release over 12 h was observed for all the compacted granules, irrespective of the drug dose. The sustained-release kinetics for 1000 mg niacin matrix tablets with Compritol 888 produced with the identified optimal parameters were similar to those for the market reference product, Niaspan® FCT 1000 mg. The tablets were stable for up to six months when stored at 25 and 40 °C. CONCLUSIONS: Wet granulation with Compritol 888 presents an effective approach to improve material flow and compressibility. High-dose lipid matrix tablets with sustained release profiles can be successfully produced.
    [Abstract] [Full Text] [Related] [New Search]